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EGFR

The epidermal growth factor receptor (EGFR; ErbB-1; HER1 in humans) is a transmembrane protein that is a receptor for members of the epidermal growth factor family (EGF family) of extracellular protein ligands.

  • Cetuximab
    T9905205923-56-4
    Cetuximab (C225) is a monoclonal antibody that is an inhibitor of human epidermal growth factor receptor (EGFR) (Kd=0.201 nM). Cetuximab has antitumor activity, inhibiting tumor cell proliferation and inducing apoptosis.
    • $197
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  • Trastuzumab
    T9912180288-69-1
    Trastuzumab is a humanized monoclonal antibody for patients with invasive breast cancers that overexpress HER2. Trastuzumab has been clinically used to treat HER2 Positive Metastatic Breast Cancer and HER2 Positive Gastric Cancer.
    • $157
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  • Sunvozertinib
    T641242370013-12-8
    Sunvozertinib (DZD9008) is a potent ErbBs and BTK inhibitor, with inhibitory effects on EGFR, Her2, and mutant epidermal growth factor. Sunvozertinib (DZD9008) showed inhibitory effects on EGFR exon 20 NPH insertion, EGFR exon 20 ASV insertion, EGFR L858R and T790M mutations, as well as Her2 exon 20 YVMA and EGFR WT A431 with IC50 of 20.4, 20.4, 1.1, 7.5, and 80.4 nM.
    • $30
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  • Osimertinib
    T24901421373-65-0
    Osimertinib (AZD-9291) is an EGFR third-generation inhibitor that inhibits the T790M resistance mutation produced by second-generation EGFR inhibitors with irreversible and oral activity. Osimertinib has antitumor activity for the treatment of EGFR-mutated non-small-cell lung cancer.
    • $32
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  • Disitamab vedotin
    T395952136633-23-1
    Disitamab vedotin (RC-48) is a newly developed antibody-active molecule conjugate (ADC) targeting human epidermal growth factor receptor 2 (HER2), consisting of hertuzumab coupled to monomethyl auristatin E (MMAE) via a cleavable linker. Disitamab vedotin showed anti-tumor and anti-proliferative activities in gastric cancer cells with different HER-2 expression levels and inhibited the expression of HER-2 protein in gastric cancer cells.
    • $347
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  • Pyrotinib dimaleate
    T125941397922-61-0In house
    Pyrotinib dimaleate is a selective EGFR HER2 dual inhibitor with IC50 values ​​of 13 and 38 nM, respectively, for the treatment of HER2-positive breast cancer.
    • $157
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  • Alflutinib mesylate
    T71752130958-55-1
    Alflutinib mesylate (AST2818 mesylate) ,is an irreversible tyrosine kinase inhibitor that selectively inhibits EGFR mutations, especially T790M.
    • $71
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  • Butein
    T6427487-52-5
    Butein is a cAMP-specific PDE inhibitor, protein tyrosine kinase inhibitor, and SIRT1 activator. It sensitizes HeLa cells to Cisplatin by targeting FoxO3a via the AKT and ERK p38 MAPK pathways.
    • $36
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  • Rilzabrutinib
    T125421575596-29-0
    Rilzabrutinib (PRN1008) is a reversible covalent, selective, and orally active inhibitor of Bruton’s Tyrosine Kinase (BTK) with an IC50 of 1.3 nM.
    • $100
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  • SDZ281-977
    T16866150779-71-8In house
    SDZ 281-977 is a derivative of Lavendustin A, an EGF receptor tyrosine kinase inhibitor.
    • $100
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  • Tucatinib
    T2364937263-43-9
    Tucatinib (ONT-380) is a potent and selective HER2 inhibitor (IC50: 8 nM).
    • $30
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  • Gefitinib
    T1181184475-35-2
    Gefitinib (ZD1839) is an EGFR first-generation inhibitor with oral activity that inhibits the EGFR 19 Del and L858R mutations. Gefitinib has antitumor activity and is used for the treatment of EGFR-mutated non-small-cell lung cancers. Gefitinib administration RESULTS in the development of the EGFR C797S resistance mutation.
    • $50
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  • Afatinib
    T21312850140-72-6
    Afatinib (BIBW 2992) is an irreversible inhibitor of the EGFR family (EGFR-wt, EGFR-L858R, EGFR-L858R T790M, and HER2) with IC50s of 0.5 nM, 0.4 nM, 10 nM, and 14 nM, respectively.
    • $30
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  • EGFR-IN-76
    T751202607829-38-7
    EGFR-IN-76 is a potent EGFR inhibitor.
    • $126
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  • Cavutilide
    T619131276186-19-6In house
    Cavutilide has antiarrhythmic activity, inhibits hERG K(+) channels, and can be used to study heart failure and persistent atrial fibrillation.
    • $293
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  • Panitumumab
    T9927339177-26-3
    Panitumumab is a fully human IgG2 monoclonal antibody targeting the epidermal growth factor receptor EGFR).
    • $178
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  • BLU-945
    T97542660250-10-0
    BLU-945 is a reversible, potent, highly selective, and orally available epidermal growth factor receptor tyrosine kinase inhibitor (TKIs). BLU-945 inhibits EGFR phosphorylation in EGFR L858R T790M C797S and EGFR ex19del T790M C797S mutant cell lines. BLU-945 can be used in lung cancer research, including non-small cell lung cancer (NSCLC).
    • $97
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  • Befotertinib
    T392751835667-63-4
    Befotertinib (D-0316) is an inhibitor of EGFR tyrosine kinase and can be used for studies about EGFR T790M-positive non-small cell lung cancer.
    • $81
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  • Epidermal Growth Factor
    T867962253-63-8
    Epidermal Growth Factor binds to epidermal growth factor receptor (EGFR) and stimulates cell growth and proliferation. It is approved for the treatment of diabetic foot ulcers.
    • $133
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  • Labuxtinib
    T798511426449-01-5
    Labutinib is a selective inhibitor of the c-kit tyrosine kinase [1].
    • $198
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  • (Rac)-JBJ-04-125-02
    T88722140807-05-0
    (Rac)-JBJ-04-125-02 (JBJ-04-125-02) is effective as a single agent in both in vitro and in vivo models of EGFR-mutant lung cancer.
    • $107
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  • Pertuzumab
    T9909380610-27-5
    Pertuzumab (anti-HER2) a humanized monoclonal antibody and the first in the class of agents called the HER2 dimerization inhibitors impairs the ability of HER2 to bind to other members of the HER family.
    • $189
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  • Osimertinib mesylate
    T36341421373-66-1
    Osimertinib mesylate (AZD-9291 mesylate) is an EGFR third-generation inhibitor that inhibits the T790M resistance mutation produced by second-generation EGFR inhibitors with irreversible and oral activity. Osimertinib mesylate has antitumor activity for the treatment of EGFR-mutated non-small-cell lung cancer.
    • $45
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  • Desmethyl Erlotinib
    T6328183321-86-0
    Desmethyl Erlotinib (CP-473420) is the active metabolite of Erlotinib (EGFR inhibitor with IC50 of 2 nM).
    • $48
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  • Almonertinib
    T54621899921-05-1
    Almonertinib (HS-10296) is an inhibitor specifically targeting EGFR activation mutations and the resistant EGFR T790M mutation, exhibiting limited activity against wild-type EGFR.
    • $91
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  • Neratinib
    T2325698387-09-6
    Neratinib (HKI-272) (HKI-272) is an orally available, irreversible tyrosine kinase inhibitor for HER2 and EGFR (IC50: 59 92 nM), respectively.
    • $30
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  • EGFR-IN-7
    T111612267329-76-8
    EGFR-IN-7 (TQB3804) is a selective and potent EGFR kinase inhibitor.
    • $98
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  • Daphnetin
    T2851486-35-1
    Daphnetin (7,8-Dihydroxycoumarin), a natural coumarin derivative, is a protein kinase inhibitor with inhibitory for EGFR (IC50: 7.67 μM), PKA (IC50: 9.33 μM), and PKC (IC50: 25.01 μM), also exhibit anti-oxidant and anti-inflammatory activities.
    • $43
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  • Erlotinib
    T0373183321-74-6
    Erlotinib (NSC-718781) is an EGFR inhibitor (IC50: 2 nM). It is used for the treatment of non-small cell lung cancer.
    • $40
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  • Genistein
    T1737446-72-0
    Genistein (NPI 031L) is a naturally occurring soy isoflavone, a multi-targeted tyrosine kinase inhibitor. Genistein has antitumor, antioxidant, and anthelmintic properties, and also produces estrogen-like effects in the body.
    • $38
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  • BGB-102
    T10531807640-87-5
    BGB-102 (JNJ-26483327) is a kinase inhibitor targeting FLT3 and YES1 and an antagonist targeting EGFR and VEGFR3, which may be useful in the study of macular degeneration and diseases associated with genetic disorders and malformations.
    • $328
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  • Lazertinib
    T44851903008-80-9
    Lazertinib (GNS-1480) is an effective, highly mutant-selective and irreversible EGFR-TKI with IC50 values of 1.7 nM, 2 nM, 5 nM, 20.6 nM and 76 nM for Del19 T790M, L858R T790M, Del19, L85R and Wild type EGFR respectively.
    • $41
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  • Dacomitinib
    T24831110813-31-4
    Dacomitinib (PF299)(PF299804; PF-00299804) is a highly selective, orally bioavailable small-molecule inhibitor of the HER family of tyrosine kinases with IC50 of 6, 45.7 and 73.7 nM for EGFR, ERBB2, and ERBB4, respectively.
    • $32
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  • Canertinib
    T6136267243-28-7
    Canertinib (CI-1033) is a pan-erbB tyrosine kinase inhibitor which work against esophageal squamous cell carcinoma in vitro and in vivo. Canertinib treatment significantly affects tumour metabolism, proliferation and hypoxia as determined by PET.
    • $31
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  • Lapatinib
    T0078231277-92-2
    Lapatinib (GW572016) is an inhibitor of ErbB2 and EGFR (IC50=9.2 10.8 nM) with oral activity. Lapatinib has antitumor activity and can be used to treat advanced or metastatic breast cancer with HER2 overexpression.
    • $29
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  • PD173074
    T2642219580-11-7
    PD173074 is an effective FGFR1 inhibitor (IC50: 25 nM) and also inhibits VEGFR2 (IC50: 100-200 nM) in cell-free assays. The selectivity is higher ~1000-fold for FGFR1 than PDGFR and c-Src.
    • $36
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  • Tarloxotinib bromide
    T130881636180-98-7
    Tarloxotinib bromide (TH-4000) is an irreversible inhibitor of EGFR HER2.
    • $143
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  • Sulforaphene
    TL0016592-95-0
    Sulforaphene is a natural product isolated from radish seeds, exhibits an ED50 against velvetleaf seedlings approximately 2 x 10 -4 M. Sulforaphene promotes cancer cells apoptosis and inhibits migration via inhibiting EGFR, p-ERK1 2, NF‐κB and other signa
    • $31
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  • WS3
    T20551421227-52-2
    WS3, a β cell proliferation inducer, regulates Erb3 binding protein-1 (EBP1) and the IκB kinase pathway.
    • $44
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  • E-4031
    T7198113559-13-0
    E-4031 is a methanesulfonanilide class III antiarrhythmic agent that prolongs cardiac action potential duration by blocking ERG K+ channels (IC50 = 29 nM)
    • $38
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  • Oritinib
    T600762035089-28-0
    Oritinib (SH-1028) is an inhibitor of EGFR with IC50s of 18, 0.7, 4, 0.1, 1.4 and 0.89 nM for EGFR (wt), EGFR (L858R), EGFR (L861Q), EGFR (L858R T790M), EGFR (d746-750), EGFR (d746-750 T790M), respectively. Oritinib can be used in studies about the treatment of non-small cell lung cancer.
    • $136
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  • Ginsenoside Rh2
    T295978214-33-2
    Ginsenoside Rh2 (20(S)-Ginsenoside Rh2), an extract of red Panax ginseng, is a potent anti-inflammatory and anticancer drug.
    • $32
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  • HKI-357
    T11569848133-17-5
    HKI-357 is an irreversible dual inhibitor of EGFR and ERBB2 (IC50s: 34 nM and 33 nM), effectively suppressing EGFR autophosphorylation (at Y1068), as well as AKT and MAPK phosphorylation.
    • $72
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  • RTC-5
    T127771423077-49-9In house
    RTC-5 (TRC-382) is a phenothiazine compound that has been specifically enhanced for its potent anti-cancer properties. It exhibits considerable effectiveness against an EGFR-driven cancer xenograft model. The mechanism behind its efficacy can be attributed to the simultaneous inhibition of PI3K-AKT and RAS-ERK signaling pathways.
    • $48
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  • 20(S)-Ginsenoside Rg3
    T340214197-60-5
    20(S)-Ginsenoside Rg3 (Rg3) possess an ability to inhibit the lung metastasis of tumor cells via inhibition of the adhesion and invasion of tumor cells. It inhibits the proliferation of human umbilical vein endothelial cells(HUVEC) and has anti-angiogenesis activities.
    • $32
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  • Icotinib
    T6153610798-31-7
    Icotinib (Conmana) is an orally available quinazoline-based inhibitor of epidermal growth factor receptor (EGFR), with potential antineoplastic activity.
    • $41
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  • TAS6417
    T169961661854-97-2
    Zipalertinib (TAS6417, CLN-081) is a novel, highly potent, orally active covalent EGFR tyrosine kinase inhibitor that uniquely binds to the ATP binding site of the EGFR hinge region with an IC50 value of 1.1-8.0 nM.
    • $89
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  • Beta-Hydroxyisovalerylshikonin
    TN14407415-78-3
    Beta-Hydroxyisovalerylshikonin is an inhibitor of protein-tyrosine kinases such as v-Src and EGFR, and has been shown to induce apoptosis in several human tumor cell lines. Beta-Hydroxyisovalerylshikonin significantly decreased viability of HCT116 cells (IC50 values = 30.9 μg mL).
    • $139
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  • BGB-8035
    T733812283349-24-4
    BGB-8035 is an orally available, selective and potent BTK inhibitor with antitumor activity that inhibits BTK, TEC and EGFR.BGB-8035 is used in the study of tumors and autoimmune diseases.
    • $413
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  • PAT-505
    T123721782070-22-7
    PAT-505 is an orally available, selective and potent inhibitor of autologous epidermal growth factor (IC50 2 nM in Hep3B cells, 9.7 nM in human blood, 62 nM in mouse plasma).
    • $299
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